Everolimus
Cat. No.:YN330057
CAS No. :159351-69-6
产品名称: | Everolimus |
CAS No.: | 159351-69-6 |
Chemical Name: | 42-O-(2-hydroxyethyl)-rapamycin |
Synonyms: | 依维莫司; RAD001; SDZ-RAD |
分子量: | 958.22 |
分子式: | C₅₃H₈₃NO₁₄ |
SMILES: | O=C([C@@]1(O)[C@@H](CC[C@@H](C[C@@H](/C(C)=C/C=C/C=C/[C@H](C[C@@H](C)C([C@@H]([C@@H](/C(C)=C/[C@H]2C)O)OC)=O)C)OC)O1)C)C(N3CCCC[C@H]3C(O[C@@H](CC2=O)[C@@H](C[C@H]4C[C@H]([C@H](OCCO)CC4)OC)C)=O)=O |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | Everolimus (RAD001) 是一种 Rapamycin 的衍生物,也是一种有效的,选择性的和口服活性的mTOR1抑制剂。Everolimus 与FKBP-12结合可产生免疫抑制复合物。Everolimus 抑制肿瘤细胞增殖并诱导细胞凋亡 (apoptosis) 和自噬 (autophagy)。Everolimus 具有有效的免疫抑制和抗癌活性。 |
IC50和靶点: | [{name:"mTOR:5-6 nM (IC50)"}] |
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Petroulakis, E., Mamane, Y., Le Bacquer, O., et al.mTOR signaling: implications for cancer and anticancer therapyBr. J. Cancer94(2),195-199(2006)
Dann, S.G., Selvaraj, A., and Thomas, G.mTOR Complex1-S6K1 signaling: At the crossroads of obesity, diabetes and cancerTrends Mol. Med.13(6),252-259(2007)
Tao, Z., Barker, J., Shi, S.D.H., et al.Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexesBiochem.49(39),8488-8498(2010)
Zeng, Z., Sarbassov, D.D., Samudio, I.J., et al.Rapamycin derivatives reduce mTORC2 signaling and inhibit AKT activation in AMLBlood109(8),3509-3512(2007)
Lebwohl, D., Anak, Ö., Sahmoud, T., et al.Development of everolimus, a novel oral mTOR inhibitor, across a spectrum of diseasesAnn. N. Y. Acad. Sci.1291,14-32(2013)
Yunokawa, M., Koizumi, F., Kitamura, Y., et al.Efficacy of everolimus, a novel mTOR inhibitor, against basal-like triple-negative breast cancer cellsCancer Sci.103(9),1665-1671(2012)
Gurk-Turner, C., Manitpisitkul, W., and Cooper, M.A comprehensive review of everolimus clinical reports: A new mammalian target of rapamycin inhibitorTransplantation94(7),659-668(2012)